E环修饰的路托品A衍生物的合成及生化性质

Synthesis and biochemical properties of E-ring modified luotonin A derivatives.

作者信息

Cagir Ali, Jones Shannon H, Eisenhauer Brian M, Gao Rong, Hecht Sidney M

机构信息

Departments of Chemistry and Biology, University of Virginia, Charlottesville, VA 22901, USA.

出版信息

Bioorg Med Chem Lett. 2004 May 3;14(9):2051-4. doi: 10.1016/j.bmcl.2004.02.069.

DOI:10.1016/j.bmcl.2004.02.069

PMID:15080977

Abstract

Luotonin A is a cytotoxic pyrroloquinazolinoquinoline alkaloid that has been shown to stabilize the human topoisomerase I-DNA covalent binary complex in the same fashion as the antitumor alkaloid camptothecin. A study of the structural elements in luotonin A required for binary complex stabilization has revealed key differences relative to those required for camptothecin.

摘要

路托品A是一种具有细胞毒性的吡咯并喹唑啉喹啉生物碱，已证明它能以与抗肿瘤生物碱喜树碱相同的方式稳定人拓扑异构酶I-DNA共价二元复合物。一项关于路托品A中稳定二元复合物所需结构元件的研究揭示了其与喜树碱所需结构元件的关键差异。